KY-05009

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

KY-05009  纯度: 99.80%

KY-05009 是一种具有 ATP 竞争性的 TNIK 抑制剂,Ki 为 100 nM。KY-05009 在药理上抑制人肺腺癌细胞中 TGF-β1 诱导的上皮-间质转化。KY-05009 还抑制 TNIK 的蛋白表达和 Wnt 靶基因的转录活性,并诱导癌细胞凋亡。KY-05009 具有抗癌活性。

KY-05009

KY-05009 Chemical Structure

CAS No. : 1228280-29-2

规格 价格 是否有货 数量
Free Sample (0.1-0.5 mg)   Apply now  
10 mM * 1 mL in DMSO ¥990 In-stock
5 mg ¥900 In-stock
25 mg ¥3600 In-stock
100 mg ¥7500 In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

KY-05009 相关产品

相关化合物库:

  • Bioactive Compound Library Plus
  • Apoptosis Compound Library
  • Immunology/Inflammation Compound Library
  • Kinase Inhibitor Library
  • MAPK Compound Library
  • Stem Cell Signaling Compound Library
  • Wnt/Hedgehog/Notch Compound Library
  • Anti-Cancer Compound Library
  • Anti-Aging Compound Library
  • Differentiation Inducing Compound Library
  • Oxygen Sensing Compound Library
  • Cytoskeleton Compound Library
  • Neuroprotective Compound Library
  • Anti-Breast Cancer Compound Library
  • Targeted Diversity Library
  • Anti-Liver Cancer Compound Library
  • Anti-Colorectal Cancer Compound Library

生物活性

KY-05009 is an ATP-competitive Traf2- and Nck-interacting kinase (TNIK) inhibitor with a Ki of 100 nM. KY-05009 pharmacologically inhibits TGF-β1-induced epithelial-to-mesenchymal transition (EMT) in human lung adenocarcinoma cells. KY-05009 inhibits the protein expression of TNIK and transcriptional activity of Wnt target genes and induces apoptosis in cancer cells. KY-05009 exerts anti-cancer activity[1].

IC50 & Target[1]

TNIK

100 nM (Ki)

体外研究
(In Vitro)

KY-05009 (0.1-30 μM; 24 hours; RPMI8226 cells) treatment inhibits the proliferation of RPMI8226 cells in a dose-dependent manner[1].
KY-05009 (1-3 μM; 48-72 hours; RPMI8226 cells) treatment induces caspase-dependent apoptosis in RPMI8226 cells in a dose-dependent manner[1].
KY-05009 (3 μM; 1 hour; RPMI8226 cells) treatment suppresses the transcriptional activity of Wnt signaling-related genes, including TNIK, CTNNB1, TCF7, and TCF4[1].
. KY-05009 (3 μM; 9 hours; RPMI8226 cells) treatment inhibits the IL-6-induced interaction between TCF4 and β-catenin and the phosphorylation of TCF4[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay[1]

Cell Line: RPMI8226 cells
Concentration: 0.1 μM, 0.3 μM, 1 μM, 3 μM, 10 μM, 30 μM
Incubation Time: 24 hours
Result: Inhibited the proliferation of RPMI8226 cells.

Apoptosis Analysis[1]

Cell Line: RPMI8226 cells
Concentration: 1 μM, 3 μM, 10 μM
Incubation Time: 48 hours, 72 hours
Result: Induced the binding of fluorescent Annexin V and 7-amino-actinomycin D (7-AAD) uptake.

RT-PCR[1]

Cell Line: RPMI8226 cells
Concentration: 3 μM
Incubation Time: 1 hour
Result: Suppressed the transcriptional activity of Wnt signaling-related genes, including TNIK, CTNNB1, TCF7, and TCF4.

Western Blot Analysis[1]

Cell Line: RPMI8226 cells
Concentration: 3 μM
Incubation Time: 9 hours
Result: The IL-6-induced interaction between TCF4 and β-catenin and the phosphorylation of TCF4 were inhibited.

分子量

352.41

Formula

C18H16N4O2S

CAS 号

1228280-29-2

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : 83.33 mg/mL (236.46 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.8376 mL 14.1880 mL 28.3760 mL
5 mM 0.5675 mL 2.8376 mL 5.6752 mL
10 mM 0.2838 mL 1.4188 mL 2.8376 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (5.90 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (5.90 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH₂O 中,得到澄清透明的生理盐水溶液

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献
  • [1]. Lee Y, et al. Synergistic inhibition effect of TNIK inhibitor KY-05009 and receptor tyrosine kinase inhibitor dovitinib on IL-6-induced proliferation and Wnt signaling pathway in human multiple myeloma cells. Oncotarget. 2017 Jun 20;8(25):41091-41101.

所有产品仅用作科学研究或药证申报,我们不为任何个人用途提供产品和服务

KY1220

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

KY1220  纯度: ≥98.0%

KY1220作用于 Wnt/β-catenin 靶点,使β-catenin 和 Ras不稳定。在HEK293报告细胞中的IC50 值为2.1 μM。

KY1220

KY1220 Chemical Structure

CAS No. : 292168-79-7

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥1380 In-stock
2 mg ¥800 In-stock
5 mg ¥1500 In-stock
10 mg ¥2500 In-stock
25 mg ¥5500 In-stock
50 mg ¥9400 In-stock
100 mg ¥16000 In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

KY1220 相关产品

相关化合物库:

  • Bioactive Compound Library Plus
  • Stem Cell Signaling Compound Library
  • Wnt/Hedgehog/Notch Compound Library
  • Anti-Cancer Compound Library
  • Anti-Aging Compound Library
  • Cytoskeleton Compound Library
  • Neuroprotective Compound Library
  • Transcription Factor Targeted Library

生物活性

KY1220 is a compound that destabilizes both β-catenin and Ras, via targeting the Wnt/β-catenin pathway; with an IC50 of 2.1 μM in HEK293 reporter cells.

IC50 & Target

IC50: 2.1 μM (HEK293 reporter cells)[1]

体外研究
(In Vitro)

KY1220 shows an IC50 of 2.1 μM in HEK293 reporter cells. KY1220 dose dependently decreases Wnt3a-CM-induced TOPflash reporter activation and mRNA expression of Wnt target genes CCND1 and MYC in HEK293 cells. In HEK293 cells, both β-catenin and panRas protein levels are similarly reduced in a dose-dependent manner after treatment with KY1220, whereas the mRNA levels of CTNNB1 (which encodes β-catenin), NRAS, KRAS and HRAS remain unchanged. K-Ras, which has a critical role in progression of CRCs, is also destabilized by KY1220 via polyubiquitin-dependent proteasomal degradation. KY1220 accelerates the degradation rates of both β-catenin and Ras in SW480 cell lines. Ras destabilization by KY1220 consequently inhibits the activities of both ERK and Akt, which are downstream effectors of Ras in SW480 cells harboring a KRAS mutation. The proliferation and transformation of the HCT15, SW480, D-WT and D-MT CRC cells are efficiently inhibited after treatment with KY1220[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

314.32

Formula

C14H10N4O3S

CAS 号

292168-79-7

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : ≥ 100 mg/mL (318.15 mM)

* “≥” means soluble, but saturation unknown.

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 3.1815 mL 15.9074 mL 31.8147 mL
5 mM 0.6363 mL 3.1815 mL 6.3629 mL
10 mM 0.3181 mL 1.5907 mL 3.1815 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

参考文献
  • [1]. Cha PH, et al. Small-molecule binding of the axin RGS domain promotes β-catenin and Ras degradation. Nat Chem Biol. 2016 Aug;12(8):593-600.

Cell Assay
[1]

HCT15 or SW480 cells are treated with 25 μM KY1220 or KYA1797K or with control (DMSO) for 72 h. Cell proliferation is measured using the MTT assay. The absorbance of the formazan product is determined at 590 nm every 24 h[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

参考文献
  • [1]. Cha PH, et al. Small-molecule binding of the axin RGS domain promotes β-catenin and Ras degradation. Nat Chem Biol. 2016 Aug;12(8):593-600.

所有产品仅用作科学研究或药证申报,我们不为任何个人用途提供产品和服务

常熟双杰E-KY系列电子天平E6KY-0.1

常熟双杰E-KY系列电子天平E6KY-0.1

  • 品牌 双杰|G&G
  • 型号 E6KY-0.1
  • 商品详情

    双杰E-KY系列电子天平E6KY-0.1

    产品特征

    1、2种称重单位:千克,磅·铝合金底座,坚固耐用

    2、计数功能(取样数:1/10/20/50/100)·应变式传感器

    3、全称量去皮·不锈钢和塑料双层秤盘

    4、自动校准·高33mm专用液晶显示器,带白色背光

    5、自带电瓶,交直流两用·可锁紧式水平调整脚

    6、RS232接口,有打印按键

    技术参数

    型号

    E3KY-0.1

    E6KY-0.1

    E15KY-0.5

    E30KY-1

    最大称量

    3kg

    6kg

    15kg

    30kg

    分辨率(d)

    0.1g

    0.1g

    0.5g

    1g

    检定分度值(e)

    10d

    10d

    10d

    10d

    去皮范围

    0~3kg

    0~6kg

    0~15kg

    0~30kg

    校准重量

    2kg

    5kg

    10kg

    20kg

    称台尺寸

    300×220mm

    体积

    330(长)×300(宽)×100(高)mm

    供电

    电源适配器输入AC220V±10%50Hz±1Hz输出DC12V/600mA

    或者充电电池DC6V/4AH/20HR

    使用温度

    0~40℃

    使用湿度

    ≤80%RH

    串口

    RS232

     

  • XDS-5KY倒置生物显微镜

    【简单介绍】

    XDS-5KY倒置生物显微镜采用优良的无限远光学系统。配置长工作距离平场物镜与大视野目镜,紧凑稳定的高刚性主体,充分体现了显微操作的防振要求。旋转摆入摆出式聚光系统,可对高培养皿或圆筒状烧瓶进行无沾染培养细胞观察。符合人机工程学要求的理想设计,使操作更方便舒适,空间更广阔。本仪器适用于对细胞组织,透明液态组织的显微观察,也可对培养皿中的培养组织进行动态显微观察。

    【详细说明】

    XDS-5KY倒置生物显微镜

    产品用途:

       XDS-5KY倒置生物显微镜采用优良的无限远光学系统。配置长工作距离平场物镜与大视野目镜,紧凑稳定的高刚性主体,充分体现了显微操作的防振要求。旋转摆入摆出式聚光系统,可对高培养皿或圆筒状烧瓶进行无沾染培养细胞观察。符合人机工程学要求的理想设计,使操作更方便舒适,空间更广阔。本仪器适用于对细胞组织,透明液态组织的显微观察,也可对培养皿中的培养组织进行动态显微观察。可应用于科研院所、高等院校、医疗卫生、检验检疫、农牧乳业等部门。

    产品特点

    观察系统-人性化设计、操作者观察更舒适。配平场广角目镜,使观察视野更广阔、舒适。

    透明载物台板-观察方便、大大降低载物台受热变形的可能

    无齿条机械载物台-配备三种不同规格的培养皿托板,适用于不同培养皿的观察。

    照明系统-一体化的照明系统,可对光源进行空间调整,以弥补灯泡的个体差异

    旋转聚光系统-可对高培养皿或圆筒状烧杯进行无粘染培养细胞观察。

    相衬观察-配置高品质的相衬平场物镜与相衬聚光镜,相衬聚光镜有拉板式与转盘式两种类型,适用于不同的操作需求。

    影慑像观察-仪器本身带有像接口、采用通光,适用于低照度的像。

    技术参数:

    目镜

    平场大视野目镜10X/Ф22mm

    对中望远镜

     无限远长工作距离平场消色差物镜

    类    型

    放大倍率

    数值孔径

    工作距离mm

    盖玻片厚度mm

    正常物镜

    10

    0.25

    19.4

    1.2

    20

    0.40

    8.0

    1.2

    40

    0.60

    3.5

    1.2

    相衬物镜

    10

    0.25

    4.3

    1.2

    目镜筒

    45°倾斜,双目瞳距调节范围:53~75mm.

    调焦机构

    粗微动同轴调焦, 微动格值:2μm,粗动松紧可调,带锁紧和限位装置

    转换器

    五孔转换器

    载物台

    固定载物台尺寸:227mmX208mm      玻璃圆载物台板尺寸:Ф118mm

    机械式移动尺寸,移动范围: 114mm*77mm

    培养皿托板一

    86mm(宽)X129.5mm(长),可适配圆形培养皿Ф87.5mm

    培养皿托板二

    34mm(宽)X77.5mm(长),可适配圆形培养皿Ф68.5mm

    培养皿托板三

    57mm(宽)X82mm(长)

    聚光系统

    特长工作距离聚光镜,工作距离55mm,带相衬装置

    照明系统

    6V30W卤素灯,亮度与空间位置可调

    滤色片

    磨砂玻璃,蓝、绿滤色片

    注:●标准配置,○选购配置